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1. (WO2007007628) CHOLINE SALT CRYSTAL OF AZULENE COMPOUND
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2007/007628 International Application No.: PCT/JP2006/313468
Publication Date: 18.01.2007 International Filing Date: 06.07.2006
IPC:
C07D 309/10 (2006.01) ,A61K 31/351 (2006.01) ,A61P 3/10 (2006.01) ,C07C 215/90 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
309
Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
02
having no double bonds between ring members or between ring members and non-ring members
08
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
10
Oxygen atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
335
having oxygen as the only ring hetero atom, e.g. fungichromin
35
having six-membered rings with one oxygen as the only ring hetero atom
351
not condensed with another ring
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
08
for glucose homeostasis
10
for hyperglycaemia, e.g. antidiabetics
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
215
Compounds containing amino and hydroxy groups bound to the same carbon skeleton
74
having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
90
with quaternised amino groups bound to the carbon skeleton
Applicants:
アステラス製薬株式会社 ASTELLAS PHARMA INC. [JP/JP]; 〒1038411 東京都中央区日本橋本町二丁目3番11号 Tokyo 3-11, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo 1038411, JP (AllExceptUS)
壽製薬株式会社 KOTOBUKI PHARMACEUTICAL CO., LTD. [JP/JP]; 〒3890697 長野県埴科郡坂城町大字坂城6351番地 Nagano 6351, Oaza-Sakaki, Sakaki-machi, Hanishina-gun, Nagano 3890697, JP (AllExceptUS)
今村 雅一 IMAMURA, Masakazu [JP/JP]; JP (UsOnly)
鈴木 貴之 SUZUKI, Takayuki [JP/JP]; JP (UsOnly)
村上 猛 MURAKAMI, Takeshi [JP/JP]; JP (UsOnly)
中西 慶太 NAKANISHI, Keita [JP/JP]; JP (UsOnly)
上林 裕始 UEBAYASHI, Hiroshi [JP/JP]; JP (UsOnly)
中村 はるか NAKAMURA, Haruka [JP/JP]; JP (UsOnly)
湯田 真道 YUDA, Masamichi [JP/JP]; JP (UsOnly)
雨ノ宮 奈穂子 AMENOMIYA, Naoko [JP/JP]; JP (UsOnly)
粟村 勇治 AWAMURA, Yuuji [JP/JP]; JP (UsOnly)
冨山 泰 TOMIYAMA, Hiroshi [JP/JP]; JP (UsOnly)
Inventors:
今村 雅一 IMAMURA, Masakazu; JP
鈴木 貴之 SUZUKI, Takayuki; JP
村上 猛 MURAKAMI, Takeshi; JP
中西 慶太 NAKANISHI, Keita; JP
上林 裕始 UEBAYASHI, Hiroshi; JP
中村 はるか NAKAMURA, Haruka; JP
湯田 真道 YUDA, Masamichi; JP
雨ノ宮 奈穂子 AMENOMIYA, Naoko; JP
粟村 勇治 AWAMURA, Yuuji; JP
冨山 泰 TOMIYAMA, Hiroshi; JP
Agent:
渡邉 一平 WATANABE, Kazuhira; 〒1110053 東京都台東区浅草橋3丁目20番18号 第8菊星タワービル3階 Tokyo 3rd Fl., No.8 Kikuboshi Tower Building, 20-18, Asakusabashi 3-chome, Taito-ku, Tokyo 1110053, JP
Priority Data:
2005-19897307.07.2005JP
Title (EN) CHOLINE SALT CRYSTAL OF AZULENE COMPOUND
(FR) CRISTAL DE SEL DE CHOLINE DE COMPOSE AZULENE
(JA) アズレン系化合物のコリン塩結晶
Abstract:
(EN) A choline salt crystal of (1S)-1,5-anhydro-1-[5-(azulen-2-ylmethyl)-2-hydroxyphenyl]- D-glucitol which shows an endothermic peak at 194 to 198°C as measured by differential scanning calorimetry (DSC analysis) and shows main peaks at about 2&thetas;(°) 5.58, 14.72, 16.80, 17.82, 21.02 and 22.46 as measured by powder X ray diffraction. Thus, a crystal of an azulene compound can be produced which is in the form of a single crystal, has a fixed quality, can be produced with good reproducibility, can be provided stably as a crystal of an active substance for use in the preparation of a pharmaceutical and is excellent in storage stability.
(FR) L'invention concerne un cristal de sel de choline de (1S)-1,5-anhydro-1-[5-(azulèn-2-ylméthyl)-2-hydroxyphényl]-D-glucitol présentant un pic endothermique à une température comprise entre 194 °C et 198 °C sur la base d'une analyse calorimétrique différentielle (analyse ACD) et des pics principaux sur une échelle 2$g(u)(°) à 5,58, 14, 72, 16,80, 17,82, 21,02 et 22,46 environ, sur la base d'une analyse par diffraction de rayons X sur poudres. L'invention permet ainsi de produire un cristal d'un composé d'azulène sous forme de monocristal, possédant une qualité fixe, pouvant être produit en série, fourni de façon stable sous forme de cristal d'une substance active, utilisé dans la préparation d'un produit pharmaceutique, et possédant une excellente stabilité de conservation.
(JA)  示差走査熱量計分析(DSC分析)で194~198°Cに吸熱ピークを有するとともに、粉末X線回折で2θ(°)5.58、14.72、16.80、17.82、21.02及び22.46付近に主ピークを有する、(1S)-1,5-アンヒドロ-1-[5-(アズレン-2-イルメチル)-2-ヒドロキシフェニル]-D-グルシトールのコリン塩結晶とすることにより、一定の品質を有する単一の結晶が再現性よく得られ、医薬の製造に用いられる原薬の結晶として安定的に供給されることが可能で、かつ、保存安定性に優れたアズレン系化合物の結晶が提供される。
front page image
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)
Also published as:
MXMX/a/2008/000247KR1020080023734EP1908757JPWO2007007628US20090182039CN101218220
CA2614545IN62/KOLNP/2008